Reacción #92103

Ecuación de reacción

Intermediate 12C

1-(2-Bromo-4-chloro-3-fluorophenyl)ethanone

tert-butyl acrylate

→

Intermediate 12D

Rendimiento 51.0%

(E)-tert-Butyl 3-(6-acetyl-3-chloro-2-fluorophenyl)acrylate

Rendimiento 51.0%

Disolventes

DMF

Condiciones de reacción

Tratamiento posterior

1. 1
   TemperaturaThe reaction was cooled to rt
2. 2
   Filtraciónfiltered
3. 3
   Concentraciónthe filtrate was concentrated
4. 4
   OtroPurification by column chromatography

Procedimiento

To a mixture of Intermediate 12C (50 g, 198 mmol), tert-butyl acrylate (50.9 g, 397 mmol) and TEA (55 mL, 397 mmol) in DMF (500 mL) was added Pd(OAc)2 (8.9 g, 39.7 mmol). The resulting mixture was stirred at 90° C. overnight. The reaction was cooled to rt, filtered, and the filtrate was concentrated. Purification by column chromatography gave Intermediate 12D (30 g, 51%) as a light yellow solid. MS (ESI) m/z: 242.7 (M+H)+.

Fuente